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Asoxime dichloride

Names

[ CAS No. ]:
34433-31-3

[ Name ]:
Asoxime dichloride

[Synonym ]:
Pralidoxime
hi-6dichloride
hj6
hi6
HI 6 Chloride

Biological Activity

[Description]:

Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR
Signaling Pathways >> Neuronal Signaling >> nAChR
Research Areas >> Neurological Disease

[Target]

IC50: acetylcholine receptors (AChRs)[1]


[In Vivo]

Asoxime dichloride (intramuscular injection into the rear limb; 2% and 0.2% of median lethal dose 15.6 and 1.56 mg/kg; 21 or 65 days) significantly improved vaccination efficacy as a dose-dependent manner when KLH is 1 mg/kg. A combination of HI-6 and keyhole limpet hemocyanin (KLH) produces a vaccination of almost the same efficacy as that for Freund's complete adjuvant[1]. Animal Model: Balb/c mice[1] Dosage: 2% and 0.2% of median lethal dose 15.6 and 1.56mg/kg Administration: Intramuscular injection into the rear limb Result: Improved vaccination efficacy at the level of immunity regulation by the nervous system.

[References]

[1]. Pohanka M, et al. HI-6 modulates immunization efficacy in a BALB/c mouse model.Environ Toxicol Pharmacol. 2013 Nov;36(3):801-6.

Chemical & Physical Properties

[ Melting Point ]:
145-147ºC

[ Molecular Formula ]:
C14H16Cl2N4O3

[ Molecular Weight ]:
359.20800

[ Exact Mass ]:
358.06000

[ PSA ]:
92.67000

[ Storage condition ]:
20°C

MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UU2990000
CHEMICAL NAME :
Pyridinium, 4'-carbamoyl-2-formyl-1,1'-(oxydimethylene)di-, dichloride, 2-oxime
CAS REGISTRY NUMBER :
34433-31-3
LAST UPDATED :
199703
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C14-H16-N4-O3.2Cl
MOLECULAR WEIGHT :
359.24
WISWESSER LINE NOTATION :
T6KJ B1UNQ A1O1- AT6KJ DVZ &G 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
819 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
295 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
168 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
451 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
333 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
476 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2100 mg/kg/14D-I
TOXIC EFFECTS :
Blood - changes in platelet count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
1960 mg/kg/14D-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Liver - changes in liver weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

MUTATION DATA

TYPE OF TEST :
Cytogenetic analysis
TEST SYSTEM :
Rodent - hamster Ovary
DOSE/DURATION :
750 mg/L
REFERENCE :
EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year: 27,152,1996

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Precursor & DownStream

Articles

Effect of reversible ligands on oxime-induced reactivation of sarin- and cyclosarin-inhibited human acetylcholinesterase.

Toxicol. Lett. 232(3) , 557-65, (2015)

Poisoning by organophosphorus compounds (OP) used as pesticides and nerve agents is due to irreversible inhibition of the enzyme acetylcholinesterase (AChE). Oximes have been widely recognized for the...

The effect of oxime reactivators on muscarinic receptors: functional and binding examinations.

Environ. Toxicol. Pharmacol. 31(3) , 364-70, (2011)

The antidotal treatment of organophosphorus poisoning is still a problematic issue since no versatile antidote has been developed yet. In our study, we focused on an interesting property, which does n...

Syntheses and in vitro evaluations of uncharged reactivators for human acetylcholinesterase inhibited by organophosphorus nerve agents.

Chem. Biol. Interact. 203(1) , 81-4, (2013)

Organophosphorus nerve agents (OPNAs) are highly toxic compounds that represent a threat to both military and civilian populations. They cause an irreversible inhibition of acetylcholinesterase (AChE)...


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